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Cytohesins are small guanine nucleotide exchange factors (GEFs) that stimulate adenosine diphosphate ribosylation factors (Arfs), GTPases which control signal transduction along various intracellular pathways. SecinH3 is a selective inhibitor of cytohesins, blocking human, mouse, and Drosophila cytohesins with IC50 values of 2.4 to 5.6 µM. It binds the Sec7 domain of these small Arf-GEFs but does not bind Sec7 domains of larger Arf-GEFs. In human liver carcinoma HepG2 cells, SecinH3 prevents cytohesin-dependent insulin signaling. In mice, SecinH3 produces hepatic insulin resistance. Inhibition of the cytohesin GEF from Drosophila, Steppke, blocks insulin signaling and interferes with development. SecinH3 is useful for studying the diverse roles of cytohesins, including the regulation of receptor-mediated cancer cell proliferation.Formal Name: N-[4-[5-(1,3-benzodioxol-5-yl)-3-methoxy-1H-1,2,4-triazol-1-yl]phenyl]-2-(phenylthio)-acetamide. CAS Number: 853625-60-2. Molecular Formula: C24H20N4O4S. Formula Weight: 460.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2)(1:3): 0.25 mg/ml, DMSO: 25 mg/ml, Ethanol: 0.3 mg/ml. lambdamax: 257 nm. SMILES: O=C(NC1=CC=C(C2=NC(OC)=NN2C3=CC=C(OCO4)C4=C3)C=C1)CSC5=CC=CC=C5. InChi Code: InChI=1S/C24H20N4O4S/c1-30-24-26-23(28(27-24)18-11-12-20-21(13-18)32-15-31-20)16-7-9-17(10-8-16)25-22(29)14-33-19-5-3-2-4-6-19/h2-13H,14-15H2,1H3,(H,25,29). InChi Key: QELIXRUQGQOCBE-UHFFFAOYSA-N.
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